Haemodynamic influence and endothelin‐1 plasma concentrations by selective or non‐selective endothelin receptor antagonists in the pig in vivo

1999 ◽  
Vol 165 (2) ◽  
pp. 163-168 ◽  
Author(s):  
HOLM ◽  
FRANCO‐CERECEDA
Keyword(s):  
Plasma Concentrations ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Endothelin 1

scholarly journals Endothelin-1, endothelin receptor antagonists, and vein graft occlusion in coronary artery bypass surgery: 20 years on and still no journey from bench to bedside

2020 ◽  
Vol 98 (9) ◽  
pp. 570-578
Author(s):  
Michael R. Dashwood ◽  
Andrzej Loesch
Keyword(s):  
Coronary Artery ◽  
Coronary Artery Bypass ◽  
Vein Graft ◽  
Graft Failure ◽  
Artery Bypass ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Endothelin 1 ◽  
Vein Graft Failure

The saphenous vein is the most commonly used bypass graft in patients with coronary artery disease. During routine coronary artery bypass, grafting the vascular damage inflicted on the vein is likely to stimulate the release of endothelin-1, a potent endothelium-derived vasoconstrictor that also possesses cell proliferation and inflammatory properties, conditions associated with vein graft failure. In both in vitro and in vivo studies, endothelin receptor antagonists reduce neointimal thickening. The mechanisms underlying these observations are multifactorial and include an effect on cell proliferation and cell/tissue damage. Much of the data supporting the beneficial action of endothelin-1 receptor antagonism at reducing intimal thickening and occlusion in experimental vein grafts were published over 20 years ago. The theme of the recent ET-16 conference in Kobe was “Visiting Old and Learning New”. This short review article provides an overview of studies showing the potential of endothelin receptor antagonists to offer an adjuvant therapeutic approach for reducing saphenous vein graft failure and poses the question why this important area of research has not been translated from bench to bedside given the potential benefit for coronary artery bypass patients.

scholarly journals The Role of Endothelin-1 and Endothelin Receptor Antagonists in Inflammatory Response and Sepsis

2014 ◽  
Vol 63 (1) ◽  
pp. 41-52 ◽  
Author(s):  
Agata Kowalczyk ◽  
Paulina Kleniewska ◽  
Michal Kolodziejczyk ◽  
Beata Skibska ◽  
Anna Goraca
Keyword(s):  
Inflammatory Response ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Endothelin 1

scholarly journals Effects of Endothelin Receptor Antagonists on the Plasma Immunoreactive Endothelin-1 Level

2000 ◽  
Vol 36 (Supplement 1) ◽  
pp. S292-S296 ◽  
Author(s):  
Terry J. Opgenorth ◽  
Jerry L. Wessale ◽  
Douglas B. Dixon ◽  
Andrew L. Adler ◽  
Samuel V. Calzadilla ◽  
...  
Keyword(s):  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Endothelin 1

Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies

2002 ◽  
Vol 103 (s2002) ◽  
pp. 112S-117S ◽  
Author(s):  
Jerry L. WESSALE ◽  
Andrew L. ADLER ◽  
Eugene I. NOVOSAD ◽  
Samuel V. CALZADILLA ◽  
Brian D. DAYTON ◽  
...  
Keyword(s):  
Amino Acid ◽  
Ex Vivo ◽  
In Vivo Studies ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Pressor Responses ◽  
Pharmacokinetic Properties ◽  
Isolated Arteries

Endothelins (ETs), 21-amino-acid peptides involved in the pathogenesis of various diseases, bind to ETA and ETB receptors to initiate their effects. Based on the same core structure, we have developed four small-molecule ET receptor antagonists, ABT-627 (atrasentan), ABT-546, A-182086 and A-192621, which exhibit differences in selectivity for ETA and ETB receptors. In this report, we compare the efficacy, potency and pharmacokinetic properties of these four antagonists, including potency in inhibiting ET-1- or Sarafotoxin 6c-induced vessel constriction in isolated arteries and efficacy in antagonizing ET-1-, big ET-1- or Sarafotoxin 6c-induced pressor responses in rats.

Sign in / Sign up

Export Citation Format

Share Document